Evidence map›Paper›PMID 40748686›Full record

ArticleJournal of medicinal chemistry2025

Discovery, Characterization, and Optimization of a Novel Positive Allosteric Modulator-Antagonist of the D

Amy E Moritz, Feijun Wang, Nora S Madaras, Amber M Kelley, Kirsten K Snyder, Disha Gandhi, Laura R Inbody, Emmanuel O Akano, Lei Shi, J Robert Lane and 3 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

0 citing papers in PubMed.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

13 authors.

Amy E MoritzMolecular Neuropharmacology Section, National Institute of Neurological Disorders and Stroke, Intramural Research Program, National Institutes of Health, 35 Convent Drive, MSC-3723, Bethesda, Maryland 20892-3723, United States.
Feijun WangCenter for Integrative Chemical Biology and Drug Discovery, UNC Eshelman School of Pharmacy, 125 Mason Farm Road, Chapel Hill, North Carolina 27599, United States.
Nora S MadarasMolecular Neuropharmacology Section, National Institute of Neurological Disorders and Stroke, Intramural Research Program, National Institutes of Health, 35 Convent Drive, MSC-3723, Bethesda, Maryland 20892-3723, United States.
Amber M KelleyCenter for Integrative Chemical Biology and Drug Discovery, UNC Eshelman School of Pharmacy, 125 Mason Farm Road, Chapel Hill, North Carolina 27599, United States.
Kirsten K SnyderMolecular Neuropharmacology Section, National Institute of Neurological Disorders and Stroke, Intramural Research Program, National Institutes of Health, 35 Convent Drive, MSC-3723, Bethesda, Maryland 20892-3723, United States.
Disha GandhiCenter for Integrative Chemical Biology and Drug Discovery, UNC Eshelman School of Pharmacy, 125 Mason Farm Road, Chapel Hill, North Carolina 27599, United States.ORCID 0000-0001-5446-8942
Laura R InbodyMolecular Neuropharmacology Section, National Institute of Neurological Disorders and Stroke, Intramural Research Program, National Institutes of Health, 35 Convent Drive, MSC-3723, Bethesda, Maryland 20892-3723, United States.
Emmanuel O AkanoMolecular Neuropharmacology Section, National Institute of Neurological Disorders and Stroke, Intramural Research Program, National Institutes of Health, 35 Convent Drive, MSC-3723, Bethesda, Maryland 20892-3723, United States.
Lei ShiComputational Chemistry and Molecular Biophysics Section, Molecular Targets and Medications Discovery Branch, National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health, 333 Cassell Drive, Baltimore, Maryland 21224, United States.ORCID 0000-0002-4137-096X
J Robert LaneDivision of Physiology, Pharmacology and Neuroscience, School of Life Sciences, Queen's Medical Centre, University of Nottingham, Nottingham NG7 2UH, U.K.ORCID 0000-0002-7361-7875
R Benjamin FreeMolecular Neuropharmacology Section, National Institute of Neurological Disorders and Stroke, Intramural Research Program, National Institutes of Health, 35 Convent Drive, MSC-3723, Bethesda, Maryland 20892-3723, United States.ORCID 0000-0002-2428-0487
Kevin J FrankowskiCenter for Integrative Chemical Biology and Drug Discovery, UNC Eshelman School of Pharmacy, 125 Mason Farm Road, Chapel Hill, North Carolina 27599, United States.ORCID 0000-0002-7173-6352
David R SibleyMolecular Neuropharmacology Section, National Institute of Neurological Disorders and Stroke, Intramural Research Program, National Institutes of Health, 35 Convent Drive, MSC-3723, Bethesda, Maryland 20892-3723, United States.ORCID 0000-0002-0624-962X

Funding

Molecular And Pharmacological Studies Of Dopamine ReceptorsZIANS002263 · NINDS · NATIONAL INSTITUTE OF NEUROLOGICAL DISORDERS AND STROKE · PI SIBLEY, DAVID · 2009 to 2025
$37.4M
University of Kansas Specialized Chemistry CenterU54HG005031 · NHGRI · UNIVERSITY OF KANSAS LAWRENCE · PI AUBE, JEFFREY · 2008 to 2013
$21.5M
Structural basis for the functions of dopamine receptors, neurotransmitter transporters, and sigma 1 receptorZIADA000606 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI SHI, LEI · 2015 to 2025
$20.5M
TO AWARD THE BASE PERIOD FOR NIMH PSYCHOACTIVE DRUG SCREENING PROGRAM (PDSP). BASE POP: 08/30/2023-08/29/2024.75N95023C00021 · NIDA · UNIV OF NORTH CAROLINA CHAPEL HILL · PI ROTH, BRYAN · 2023 to 2025
$9.0M
Molecular &Pharmacological Studies Of Dopamine ReceptorZ01NS002263 · NINDS · NEUROLOGICAL DISORDERS AND STROKE · PI SIBLEY, DAVID R. · 1985 to 2008
$3.1M
Negative allosteric modulators of the D3 dopamine receptor as therapeutic leads for substance use disordersUG3DA050820 · NIDA · UNIV OF NORTH CAROLINA CHAPEL HILL · PI FRANKOWSKI, KEVIN J. · 2021 to 2022
$428k
Intramural NIH HHS Z01 NS002263Intramural NIH HHS ZIA DA000606Intramural NIH HHS ZIA NS002263NHGRI NIH HHS U54 HG005031NIDA NIH HHS 75N95023C00021NIDA NIH HHS UG3 DA050820
6 · The paper itself

Abstract

To identify novel D3 dopamine receptor (D3R)-selective antagonist scaffolds, we conducted a high-throughput screen of a small-molecule library using a β-arrestin recruitment assay. The lead hit compound,

Indexed as

Dopamine AntagonistsDrug DiscoveryReceptors, Dopamine D3Allosteric RegulationAnimalsbeta-ArrestinsHEK293 CellsHigh-Throughput Screening AssaysHumansMaleMiceStructure-Activity Relationshipbeta-ArrestinsDopamine AntagonistsReceptors, Dopamine D3

Identifiers

PMID40748686
PMCPMC12327755

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.